Design, synthesis and exploration of novel triazinoindoles as potent quorum-sensing inhibitors and radical quenchers.
Future Med Chem
; 16(5): 399-416, 2024 03.
Article
in En
| MEDLINE
| ID: mdl-38375563
ABSTRACT
Background:
Antimicrobial resistance has become a critical health concern, and quorum-sensing exacerbates the resistance by facilitating cell-to-cell communication within the microbial community, leading to severe pathogenic outbreaks. Methods &results:
Novel 1-(2-((5H-[1,2,4]-triazino[5,6-b]indol-3-yl)thio)acetyl)indoline-2,3-diones were synthesized. The title compounds exhibit outstanding anti-quorum-sensing efficacy, and compound 7g demonstrated the maximum proficiency (IC50 = 0.0504 µg/ml). The hybrids displayed potent antioxidant action, and compound 7c showed the highest antioxidant ability (IC50 = 40.71 µg/ml). Molecular docking of the isatin hybrids against DNA gyrase and quorum-sensing receptor CviR validated the observed in vitro findings. The befitting pharmacokinetic profile of the synthesized drug candidates was ascertained through absorption, distribution, metabolism, excretion and toxicity screening.Conclusion:
The remarkable biocompetence of the synthesized triazinoindoles may help to combat drug-resistant infections.Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Anti-Infective Agents
/
Anti-Bacterial Agents
Language:
En
Journal:
Future Med Chem
Year:
2024
Type:
Article
Affiliation country:
India